University of Szeged, Interdisciplinary Excellence Centre, Department of Physical Chemistry and Materials Science, H-6720, Rerrich B. Square 1, Szeged, Hungary.
University of Szeged, Interdisciplinary Excellence Centre, Department of Physical Chemistry and Materials Science, H-6720, Rerrich B. Square 1, Szeged, Hungary; MTA Premium Post Doctorate Research Program, University of Szeged, Hungary.
Colloids Surf B Biointerfaces. 2019 Apr 1;176:212-218. doi: 10.1016/j.colsurfb.2019.01.012. Epub 2019 Jan 3.
Three drugs with different hydrophilicity are encapsulated in poly-lactide (PLA) and Poly(lactide-co-glycolide) (PLGA) drug delivery systems prepared by ring-opening polymerization (ROP). Formation of well-defined core-shell type nanoparticles (NPs) is observed for α-tocopherol (TP) and by systematically altering the hydrophilicity of the drug carrier NPs the entrapment efficiency (EE (%)) can be remarkably controlled. The highest (90%) of EE (%) is obtained for the most lipophilic TP from the applied three drugs in the 75% lactide-containing PLGA75 NPs, which is ca. 69% for PLA NPs. Subsequent to drug loading the detailed characterization of the polymers and the formed NPs was carried out. Precipitation titrations reveal that our PLGAs have narrower weight distribution than the commercially available polymer enabling favorable properties to obtain NPs with better size distribution. It is pointed out that during the synthesis the applied solvent and stabilizing agent play a decisive role in the size distribution and stability of the drug carrier NPs. The Pluronic F127-stabilized NPs have the smallest diameter (ca. 190 nm) with less polydispersity among the applied stabilizing agent in nanoprecipitation.
三种亲水性不同的药物被包裹在聚乳酸（PLA）和聚（乳酸-共-乙醇酸）（PLGA）药物输送系统中，这些系统是通过开环聚合（ROP）制备的。观察到α-生育酚（TP）形成了明确的核壳型纳米颗粒（NPs），并且通过系统地改变药物载体 NPs 的亲水性，可以显著控制包封效率（EE（%））。在所应用的三种药物中，最亲脂性的 TP 在 75%丙交酯含量的 PLGA75 NPs 中获得了最高（90%）的 EE（%），而 PLA NPs 则为 69%。药物负载后，对聚合物和形成的 NPs 进行了详细的表征。沉淀滴定表明，与市售聚合物相比，我们的 PLGA 具有更窄的分子量分布，从而能够获得具有更好粒径分布的 NPs，从而获得更好的性能。有人指出，在合成过程中，所应用的溶剂和稳定剂在药物载体 NPs 的粒径分布和稳定性方面起着决定性的作用。在纳米沉淀中，使用 Pluronic F127 稳定的 NPs 的直径最小（约 190nm），分散性也最小。
